ABSTRACT
The present work aims to enhance the water solubility of nimodipine, a hydrophobic drug, using a solid dispersion(SD) technique. Soluplus® as a novel hydrophilic polymeric carrier was used. Nimodipine-Soluplus® SDs (1:10) wereprepared by impregnation technique using supercritical fluid technology (SCF) and compared with the ones whichwere prepared by conventional hot-melt (HM) method. The solubility and the in vitro release study of the raw drug,solid dispersions, and the corresponding physical mixtures were characterized and compared. The prepared SD bySCF technology showed 77-fold increase in nimodipine solubility, in comparison to 48-fold increase when preparedby HM and 7.7-fold when physically mixed. Moreover, they showed the highest percentage of nimodipine cumulativerelease within the studied period. The results were confirmed the amorphous transfer of the drug into the polymermatrix which was assured by the powder X-ray diffraction and the thermal analysis. In addition to the hydrogen bondformation between nimodipine and Soluplus®, which was evident in the FTIR spectra; A weakening of peak related tonimodipine N–H stretching and C=O of the ester group. Nimodipine solid dispersion with Soluplus® using the SCFtechnology might represent a promising formulation for nimodipine to enhance its oral bioavailability
ABSTRACT
In this work, the potential of using microspherical aerogel particles based on commercial carrageenan as a drug vehiclewas evaluated. Carrageenan hydrogel microparticles were prepared following the emulsion gelation approach. Afterthe successive solvent exchange, supercritical CO2 drying procedure was employed to obtain aerogel microsphericalparticles. Meloxicam and atorvastatin (class II drug) were loaded into the aerogel matrix by adsorption from theircorresponding supercritical CO2 solution. All preparations were characterized by their physicochemical properties. Invitro drug released was investigated for the drug-aerogel formulation to assist the effect of aerogel technology on therelease profile of the targeted drug. Meloxicam and atorvastatin model drugs maintained their crystalline structure.Significant enhancement in the release profile of meloxicam after loading in the carrageenan aerogel can be related tode-aggregation of meloxicam inside the particle, while no enhancement in atorvastatin release was observed. Resultswere indicative of a failure in the loading of atorvastatin inside the carrageenan particle at the selected experimentalprocessing parameters.